Nicardipine
Mechanism :
Nicardipine is a calcium channel blocker, which inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. The effects of nicardipine HCl are more selective to vascular smooth muscle than cardiac muscle.
Indication :
Contraindications :
Nicardipine is contraindicated in patients with hypersensitivity to the drug, in patients with advanced aortic stenosis. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance. Caution In liver impairment, extensively metabolised by liver. May cause decrease in GFR.
Dosing :
Not approved by FDA for pediatric use.
Continuous IV infusion initially 500 ng/kg/min followed by maintenance infusion of 1-4 mcg/kg/min.
Adverse Effect :
Commonly reported adverse effects are headache, flushing, tachycardia, palpitations, dizziness, rash, gum hyperplasia. May increase intracranial pressure.
Interaction :
Beta-blockers: May increase cardiovascular adverse effects.
Cimetidine: May increase nicardipine serum concentration.
Digoxin: May increase digoxin serum concentration; monitor digoxin levels and if necessary, reduce digoxin dose.
Rifampicin: Do not use together as effective levels of nicardipine may not be reached.
Bioavailability is increased if taken with grapefruit juice.
Fentanyl: Severe hypotension has been reported during fentanyl anesthesia with concomitant use of a beta-blocker and a calcium channel blocker.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function. Start with small doses |
| <10 | Dose as in normal renal function. Start with small doses |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HD | Not dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in GFR=10–20 mL/min |
Hepatic Dose :
Use caution in patients with hepatic impairment or reduced hepatic blood flow. Start with the lowest dose and extend the dosing interval based on clinical response.